| Description | Firsocostat (GS-0976) is an inhibitor of acetyl-CoA carboxylase (ACC) dimerization that inhibits human ACC1 and ACC2 activity (IC50s of 2.1 and 6.1 nM, respectively) |
| In vitro | ND-630 inhibited hACC1 with an IC50 of 2.1 ± 0.2 nM and hACC2 with an IC50 of 6.1 ± 0.8 nM .?Inhibition was reversible and highly specific for ACC, as evidenced by the absence of an effect of ND-630 on the activity of 101 enzymes, receptors, growth factors, transporters, and ion channels of the Ricerca DrugMatrix Panel at 10 μM .?In addition, because the ACC dimerization site is not conserved among the mammalian carboxylases , ND-630 lacks the ability to inhibit any of these mechanistically related enzymes and therefore exhibits absolute specificity for ACC inhibition relative to other mammalian carboxylases. |
| In vivo | ND-630 reduces hepatic steatosis in a rat model of diet-induced obesity and in Zucker diabetic rats. It also improves insulin secretion stimulated by glucose and reduces hemoglobin A1c levels by 0.9% in Zucker diabetic rats. |
| Target activity | ACC1:2.1 nM , ACC2:6.1 nM |
| Synonyms | ND-630, NDI-010976, GS-0976 |
| molecular weight | 569.63 |
| Molecular formula | C28H31N3O8S |
| CAS | 1434635-54-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (105.33 mM) |
| References | 1. Harriman G , Greenwood J , Bhat S , et al. Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats[J]. Proceedings of the National Academy of Sciences, 2016:201520686. |
| Citations | 1. Li M, Yang J, Ye C, et al. Integrated Metabolomics and Transcriptomics Analyses Reveal Metabolic Landscape in Neuronal Cells during JEV Infection. Virologica Sinica. 2021: 1-12. |